| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
beta-adrenoceptor
|
|---|---|
| ln Vitro |
It is not recommended to use bambuterol ((±)-Bambuterol; KWD-2183) in pregnant women or those with significantly reduced liver function. People with renal impairment can use it, but they must modify the dosage. comparable to albuterol, babuterol can have comparable adverse effects, such as headache, dizziness, tremor, weariness, nausea, and palpitations in the heart.
|
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
The bioavailability after oral administration is 20%. Metabolism/Metabolites Primarily metabolized in the liver. Further metabolized to terbutaline by plasma cholinesterase. Biological Half-Life Bambuterol has a half-life of 13 hours, while the main active metabolite, terbutaline, has a half-life of 21 hours. |
| References | |
| Additional Infomation |
Bambuterol is a carbamate, a derivative of terbutaline, with both of its phenolic hydroxyl groups protected as the corresponding N,N-dimethylcarbamates. It is a long-acting β-adrenergic receptor agonist used to treat asthma and is a prodrug of terbutaline. It has multiple functions, including β-adrenergic agonist, prodrug, bronchodilator, anti-asthmatic, EC 3.1.1.7 (acetylcholinesterase) inhibitor, sympathomimetic agent, and uterine contraction inhibitor. It is a carbamate belonging to the phenylethanolamine class of compounds. Its function is related to terbutaline. It is a prodrug of terbutaline.
Drug Indications For the prevention and reversal of bronchospasm in patients aged 12 years and older with asthma and in patients with reversible bronchospasm associated with bronchitis and emphysema. Mechanism of Action The pharmacological action of bambuterol is at least partly attributed to its stimulation of intracellular adenylate cyclase via β-adrenergic receptors (β2 receptors), an enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic adenosine monophosphate (cAMP). Elevated cAMP levels are associated with bronchial smooth muscle relaxation and the release of immediate-type hypersensitivity mediators from inhibitory cells, particularly mast cells. Pharmacodynamics Bambuterol is a long-acting β2-adrenergic receptor agonist used to treat asthma. It is a prodrug of terbutaline. Bambuterol causes smooth muscle relaxation, thereby dilating the bronchi. |
| Molecular Formula |
C18H29N3O5
|
|---|---|
| Molecular Weight |
367.44
|
| Exact Mass |
367.211
|
| CAS # |
81732-65-2
|
| Related CAS # |
Bambuterol hydrochloride;81732-46-9;Bambuterol-d9 hydrochloride;1794810-59-5
|
| PubChem CID |
54766
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.154 g/cm3
|
| Boiling Point |
500.9ºC at 760 mmHg
|
| Flash Point |
256.7ºC
|
| LogP |
2.619
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
26
|
| Complexity |
446
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(N(C)C)OC1C=C(C(CNC(C)(C)C)O)C=C(OC(N(C)C)=O)C=1
|
| InChi Key |
ANZXOIAKUNOVQU-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C18H29N3O5/c1-18(2,3)19-11-15(22)12-8-13(25-16(23)20(4)5)10-14(9-12)26-17(24)21(6)7/h8-10,15,19,22H,11H2,1-7H3
|
| Chemical Name |
[3-[2-(tert-butylamino)-1-hydroxyethyl]-5-(dimethylcarbamoyloxy)phenyl] N,N-dimethylcarbamate
|
| Synonyms |
Bambuterol; 81732-65-2; Bambuterolum; CHEBI:553827; Y1850G1OVC; [3-[2-(tert-butylamino)-1-hydroxyethyl]-5-(dimethylcarbamoyloxy)phenyl] N,N-dimethylcarbamate; (+-)-5-(2-(tert-Butylamino)-1-hydroxyethyl)-m-phenylene bis(dimethylcarbamate); DTXSID5048550;
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7215 mL | 13.6077 mL | 27.2153 mL | |
| 5 mM | 0.5443 mL | 2.7215 mL | 5.4431 mL | |
| 10 mM | 0.2722 mL | 1.3608 mL | 2.7215 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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